The solution of vinpocetine

 

(57) Abstract:

The invention relates to the field of pharmaceutical industry and relates to a medicinal product of Vinpocetine. The invention lies in the fact that the pharmaceutical composition comprises a solution of Vinpocetine, succinic acid, excipients, as auxiliary substances contains: sodium chloride, sodium, peruserdictionary, ascorbic acid, water at a content of ingredients. The invention provides high solubility of Vinpocetine in the water. 1 C.p. f-crystals, 1 table.

The invention relates to medicine, specifically to drug with antiaggregatory, antihypoxic, improves cerebral circulation, vasodilator - Vinpocetine.

Vinpocetine - ethyl ester apovincaminate acid, is a semisynthetic derivative alkaloid of devineni contained in the plant the small periwinkle.

The drug combines vascular and metabolic actions. Expands the blood vessels of the brain, increases blood flow, mainly in ischemic areas, improves the supply of oxygen to the brain, promotes glucose utilization and increases the level of catecholamines in the Central nervous system is a, atherosclerotic changes in blood vessels of the brain), memory disorders, musculoskeletal disorders, aphasia and dizziness, headache, etc. In ophthalmology Vinpocetine used in atherosclerotic and angiospastic changes net and vascular membranes, degenerative changes yellow spots, with secondary glaucoma associated with partial thrombosis of vessels, etc. also Apply to the decrease in vascular hearing or toxic origin.

Release the drug in pill form, as well as solutions (Mashkovsky, M. D. "Medicines), LLC "New wave", 2002,, I. I, S. 390-391), however, information about the composition of the solution in open publications are scarce. At the same time, the use of a solution of Vinpocetine is very effective in acute stroke: accelerates the regression of cerebral and focal symptoms, improves memory, attention, intellectual productivity. Therefore, the development of the pharmaceutical composition of Vinpocetine in the form of a solution is important.

In addition, the Russian market insufficiently provided with this drug, in addition Vinpocetine very costly because of the necessity to buy drug abroad.

The patent is down syndrome, with the use of Vinpocetine, however, the composition of the solution in the patent is not given.

In U.S. patent No. 4749707, 1988, describes the solution of Vinpocetine in aqueous or aqueous-alcoholic medium in the form of a citric acid salt of Vinpocetine.

The disadvantage of this dosage form is the low solubility of citrate in water, and therefore add alcohol, for example, benzyl, which is the preservative solution.

The objective of the invention is the creation on the basis of a more soluble derivative of Vinpocetine solution of Vinpocetine that meets all the requirements of Gosfarmakapei XI edition.

This is achieved by using instead of Vinpocetine citrate succinate of Vinpocetine in which succinic acid is used as a reagent, a solvent, providing high solubility of Vinpocetine in the water. Earlier in the Vinpocetine succinic acid was not used.

Used in composition with Vinpocetine succinic acid also improves the pharmacological properties of Vinpocetine as succinic acid as a natural metabolite in the body, increases energy metabolism in various organs and tissues of the body, including porajennyh, than benzyl alcohol preservative - sodium, peruserdictionary.

The proposed solution contains Vinpocetine Vinpocetine, succinic acid, sodium chloride, sodium, peruserdictionary, ascorbic acid in the following ratio, wt.%:

Vinpocetine 0,25-1,0

Succinic acid 0,165-1,5

Sodium chloride 0,088-0,092

Sodium, peruserdictionary 0,2-0,5

Ascorbic acid 0,05-0,5

Water Up to 1000 ml

The resulting solution of Vinpocetine meets all the requirements of Gosfarmakapei USSR XI publications and regulatory requirements for drug Vinpocetine (see table) and retains its stability for a period of not less than two years (in accordance with the requirements of the medicines).

The following examples illustrate the invention.

Example 1. In the flask is charged with 800-850 ml of sterile water for injection, add sequentially 10.0 g of succinic acid, 9.0 g of sodium chloride, 5.0 g of sodium preservestacktrace, 0.5 g of ascorbic acid and 5.0 g of Vinpocetine. The mass is stirred until complete dissolution of the components, the volume was adjusted to 1000 ml of a Solution of Vinpocetine is subjected to sterilizing filtration and dispensed in ampoules of 2 ml Gender is e solution of Vinpocetine carried out as in example 1, on the basis of 1,65 g of succinic acid, 2.5 g of Vinpocetine, 5.0 g of ascorbic acid, 0.88 g of sodium chloride, 4.8 g of sodium preservestacktrace. Get solution of Vinpocetine, which meets all regulatory requirements (see table).

Example 3. Obtaining a solution of Vinpocetine carried out as in example 1, on the basis of 15 g of succinic acid, 10 g of Vinpocetine, and 9.1 g of sodium chloride, 2 g of sodium preservestacktrace, 3 g of ascorbic acid. Get solution of Vinpocetine, which meets all regulatory requirements (see table).

1. The solution of Vinpocetine containing reagent-solvent and excipient, characterized in that, as a reagent, a solvent it contains succinic acid in the following ratio, wt.%, in 1000 ml of water:

Vinpocetine 0,25-1,0

Succinic acid 0,165-1,5

Excipients 0,338-1,092

2. The solution of Vinpocetine on p. 1, characterized in that as auxiliary substances it contains sodium chloride, sodium, peruserdictionary, ascorbic acid and water in the following ratio, wt.%:

Sodium chloride 0,088-0,092

Sodium, peruserdictionary 0,2-0,5

Ascorbic acid 0,05-0,5


 

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